Dr. Jin Google Scholar Citations
2025
Xu, Z.; Pokushalov, D.; Kabir, M.; Lee, Y.; Chattopadhyay, M.; Jenkins, E. C.; Choo, C.; Kaniskan, H. Ü.; Germain, D.*; Jin, J.*“Targeting the Mitochondrial Protease ClpP for Anticancer Therapy”. Journal of Medicinal Chemistry, 2025, 68(20):21377-21393. PMID: 41032690.
Nelson, T.; Kemper, R.; Chiarella, A.; Gonzalez, T. S.; Carroll, M.; Tripathi, S.; Clarke, B.; Yu, X.; Hu, X.; Cooke, A.; Chirumamilla, B.; Chandler, A.; McGilvary, E.; Pattenden, S.; Jin, J.; Crona, D.*; Hathaway, N.* “A first-in-class chemical-induced proximity system achieves dose-dependent control of Tumor Protein 53 (TP53) gene activation in preclinical models of gastric cancer”, ACS Pharmacology & Translational Science, 2025, 8(10):3585-3599. PMCID: PMC12519258.
Dutta, R. P.; Lee, H. H.; Leshchenko, V. V.; Shukla, R. P.; Yan, F.; Liu, Y.; Kaniskan, H. Ü.; Qiu, X.; Jin, J.; Alinari, L.; Wang, M.; Parekh, S.* “SOX11 Modulates BCR Signaling Through the PAX5/CD19 Axis for Therapeutic Targeting in BTK Resistant Mantle Cell Lymphoma”, Blood Advances, 2025, doi: 10.1182/bloodadvances.2025016801. PMID: 40845256.
Chen, L.; Deng, Z.; Xiong, Y.; Liu, J.; Huang, D.; Wang, J.; Chen, Y.; Inuzuka, H.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.* “Deubiquitinase-Targeting Chimeras Mediated Stabilization of Tumor Suppressive E3 Ligase Proteins as a Strategy for Cancer Therapy”. Journal of the American Chemical Society, 2025, 147(33):29875-29883. PMCID: PMC12395470.
Hu, X.; Graciano, K.; Hu, J.; Liu, C.; Zhang, J.; Xie, L.; Chen, X.; Xiong, Y.; Jin, J.*; Xu, J.* “Discovery of the first-in-class Aurora B kinase selective degrader” European Journal of Medicinal Chemistry, 2025, 298: 118006. PMCID: PMC12379206.
Yum, C.; Schaefer, R.; Wang, R.; Wang, T.; Lu, X.; Liu, Q.; Ren, Y.; Meng, Q.; Yang, Y.; Zhang, X.; Xiong, Y.; Yu, X.; Zhang, X.; Jin, J.; Dong, X.; Yi, Y.; Yang, R.; Cao, Q.* “Ketone drink enhances therapeutic efficacy in prostate cancer by targeting EZH2”, Oncogenesis, 2025, 14(1):24. PMCID: PMC12255682.
Zhu, S.; Gao, H.; Jiang, D.; Guo, G.; Hou, J.; Han, Y.; Zhang, C.; Hu, X.; Indulkar, S.; Kloeber, J. A.; Hu, Q.; Jiang, Y.; Zeng, X.; Ouyang, Y.; Lu, J.; Yin, P.; Luo, K.; Huang, J.; Wu, Z.; Chen, B.; Xiao, H.; Dragojevic, S.; Qin, H.; Zhou, X.; Jin, J.; Tu, X.; Wang, L.; Luo, Z.* “Isoform-Specific Function of NSD3 in DNA Replication Stress Confers Resistance to PARP Inhibitors in Prostate Cancer”, Molecular Cell, 2025, 85(14):2673-2687.e8. PMCID: PMC12276998.
Hosseini, A.; Qiu, X.; Xiong, Y.*; Chiang, K. H. N.; Catlett, J.; Kaltheuner, I.; Deng, Z.; Ghosh, S.; Shi, Y.*; Jin, J.* “Discovery of an LSD1 PROTAC Degrader”, Proceedings of the National Academy Sciences of the United States of America (PNAS), 2025, 122(20):e2425812122. PMCID: PMC12107161.
Qian, C.; Wang, Z.; Xiong, Y.; Zhang, D.; Zhong, Y.;Inuzuka, H.; Qi, Y.; Xie, L.; Chen, X.; Wei, W.* ; Jin, J.* , “Harnessing the Deubiquitinase USP1 for Targeted Protein Stabilization”. Journal of the American Chemical Society , 2025, 147(17):14564-14573. PMCID: PMC12077936.
Zhong, Y.; Kim, H. S.; Qian, C.; Xie, L.; Chen, X.; Xiong, Y.; Hu, J.; Chen, M.; Guccione, E.; Shen, Y.*; Jin, J.* , “Discovery of A Potent and Selective Protein Arginine Methyltransferase 5 (PRMT5) PROTAC Degrader”. Journal of Medicinal Chemistry, 2025, 68(8): 8543–8563. PMCID: PMC12080994.
Deng, Z.; Catlett, J.; Lee, Y.; Wu, Q.; Xu, Z.; Xie, L.; Chen, X.; Xiong, Y.; Kaniskan, H. U.*; Jin, J.*; “Harnessing the SPOP E3 Ubiquitin Ligase via Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation”, Journal of Medicinal Chemistry, 2025, 68(8):8634-8647. PMCID: PMC12043353.
Yim, H.; Sun, R.; Xu, Z.; Kim, H. S.; Kim, M.; Cao, T.; Xie, L.; Chen, X.; Kaniskan, H. U.*; Jin, J.*; “Discovery of the First-in-class DOT1L PROTAC Degrader” European Journal of Medicinal Chemistry , 2025, 291:117595. PMCID: PMC12045715.
Qian,C.; Lee,Y.; Han,Y.; Zhong,Y.; Zhou,J.; Hrit, J.; Xie,L.; Chen, Q.; Kaniskan, H. U.; Chen, X.; Rothbart, S.; Cheng, X.; Xiong, Y.*; Jin, J.* , “Structure-activity Relationship Studies of DNA Methyltransferase 1 (DNMT1) Monovalent Degraders”. Journal of Medicinal Chemistry, 2025, 68(3):2903–2919. PMCID: PMC11932022.
Deng, Z; Chen, L; Qian, C; Liu,J; Wu,Q; Song,X; Xiong,Y.; Wang, Z; Hu, X; Inuzuka, H; Zhong, Y; Lin; Y; Pham, N.D.; Shi,Y; Wei ;W.*; Jin,J.* Angewandte Chemie International Edition, “The First-in-class Deubiquitinase-targeting Chimera Stabilizes and Activates cGAS.”,2025, 64(3):e202415168. PMCID: PMC11738674.
Kabir. M.; Hu, X. Martin, T. C.; Pokushalov, D.; Kim, Y. J.; Chen, Y.; Zhong, Y.; Wu, Q; Chipuk, J. Y.; Shi, Y; Xiong, Y.; Gu, W.; Parsons, R. E.; and Jin, J.* , “Harnessing the TAF1 Acetyltransferase for Targeted Acetylation of the Tumor Suppressor p53”, Advanced Science, 2025, 12(7):e2413377. PMCID: PMC11831463.
Wang, Z.; Qian, C.; Xiong, Y.; Zhang, D.; Inuzuka, H.; Zhong, Y.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.*, “USP28-Based Deubiquitinase-Targeting Chimeras for Cancer Treatment”, Journal of the American Chemical Society,2025, 147(16):13754–13763. PMCID: PMC12105324.
Zhu, Z.; Chen, H.; Qiu, X.; Kaniskan, H. Ü.; Xie, L.; Chen, X.; Jin, J.*; Liu, P.* “(GGAA)3-based TF-PROTACs enable targeted degradation of ETV6 to inhibit Ewing sarcoma growth”, Journal of the American Chemical Society, 2025, 147(16):13396–13404. PMID: 40215343.
Teichman , E. M.; Hu , J.; in, H.; Fisher, R. F.; Blando, A.; Hu, X.; Kaniskan , H. U; Montgomery, S. E.; Cai, M.; Parise, L.; Wang, J.; Russo, S.; Han, M.*; Jin , J.*; Morel, C.* , “Design and validation of novel brain-penetrant HCN channel inhibitors to ameliorate social stress-induced susceptible phenotype”. Molecular Psychiatry, 2025, 30(9):3937-3950.PMCID: PMC12339378.
Xie, L; Sheehy, RN; Muneer, A; Xiong, Y; Wrobel, JA; Zhang, F; Park, KS; Velez, J; Liu, J; Luo, YJ; Asrican, B; Dong, P; Li, YD; Damian, C; Quintanilla, L; Li, Y; Xu, C; Deshmukh, M; Coleman, LG Jr; Ming, GL; Song, H; Wen, Z; Jin, J*; Song, J*; Chen, X*. “Development of a brain-penetrant G9a methylase inhibitor to target Alzheimer’s disease-associated proteopathology”. Nature Communication, 2025. 16(1):4222. PMCID: PMC12056044.
Yu, Y.; Yu, X.; Pan, B.; Chan, H. M.; Kaniskan, H. Ü.; Jin, J.; Cai, L.*; Wang, G. G.*, “Pharmacologic degradation of WDR5 suppresses oncogenic activities of SS18::SSX and provides a therapeutic of synovial sarcoma”. Science Advances , 2025, 11:eads7876. PMCID: PMC12017321.
Wang, SE; Cheng, Y; Lim, J; Jang, MA; Forrest, EN; Kim, Y; Donahue, M; Jo, S; Qiao, SN; Lee, DE; Hong, JY; Xiong, Y; Jin, J; Wang, S; Jiang, YH. “Mechanism of EHMT2-mediated genomic imprinting associated with Prader-Willi syndrome”. Nature Communication, 2025, 16(1):6125. PMCID: PMC12229668.
Tiedje, V.; Greenberg, J.; Qin, T.; Im, S. Y.; Krishnamoorthy, G. P.; Boucai, L.; Xu, B.; French, J. D.; Sherman, E. J.; Ho, A. L.; de Stanchina, E.; Socci, N. D.; Jin, J.; Ghossein, R. A.; Knauf, J. A.; Koche, R. P.; Fagin, J. A.* “Loss of tumor cell MHC class II drives MAPK inhibitor insensitivity of BRAF-mutant anaplastic thyroid cancers” The Journal of Clinical Investigation, 2025, 135(20): e191781. PMCID: PMC12520682.
Atienza Párraga, A.; Nylund, P.; Diamanti, K.; Garrido-Zabala, B.; Tziola, S. I.; Vasquez, L.; Pyl, P. T.; Raykova, D.; Skaftason, A.; Ma, A.; Jin, J.; Martín-Subero, J. I.; Öberg, F.; De Bruyne, E.; Komorowski, J.; Jernberg Wiklund, H.*; Kalushkova, A.* “Combinatorial DNMTs and EZH2 inhibition reprograms the H3K27me3 and DNAme-mediated onco-epigenome to suppress multiple myeloma proliferation” Scientific Reports, 2025, 15(1):31568. PMCID: PMC12391466.
Haspula, D.; Cui, Z.; Pittala, S.; Cui, Y.; Lu, H.; Xiong, Y.; Jin, J.; Gavrilova, O.; Hwang, E.; Ajwani, J.; Portillo, B.; Williams, K. W.; Inoue, A.; Weiss, J.* “G proteins of the G12 family expressed by POMC neurons regulate key metabolic functions” Science Advances, 2025, 11(28):eadu1670. PMCID: PMC12248387.
Martinez, Criseyda; Xiong, Yan; Bartkowski, Alison; Harada, Ibuki; Ren, Xiaoxiao; Byerly, Jessica; Port, Elisa; Jian Jin*; Irie, Hanna*. “A PROTAC degrader suppresses oncogenic functions of PTK6 inducing apoptosis of breast cancer cells”, Cell Chemical Biology, 2025, 32(2):255-266.E8. PMCID: PMC11845306.
Gumpper, R. H.*; Jain, M. K.; Kim, K.; Sun, R.; Sun, N.; Xu, Z.; DiBerto, J. F.; Krumm, B. E.; Kapolka, N. J.; Kaniskan, H. U.; Nichols, D. E.; Jin, J.; Fay, J. F.; Roth, B. L.* “The Structural Diversity of Psychedelic Drug Actions Revealed”, Nature Communications, 2025, 16:2734. PMID: 40108183.
H, Su; Sun, Y; Han, G; Chen, S; Liu, S; Gao, A; Zhao, R; Glen, R; Jin, J; Qu, C; Yu, M; Klug, C.; K., A.; Zheng, G., Y.; Ballinger, S.; Kutny, M.; Chen, Y.; Luo, M*; Zhao, X.*, “PRMT1-Mediated Metabolic Reprogramming Promotes Leukemogenesis”. eLife, 2025, 14: RP105318. PMCID: PMC12349897.
Bauer, L.G., Ward, J.A., Díaz-Sáez, L., Sundström, Y., Tolvanen, T., Barrera, J. C. A., Kostidis, S., Rogers, C.M., Panagakou, I., Singh, U., Rothweiler, E.M., Gonzalez, Orta A, Kaniskan, H. Ü., Hu, J., Jin, J., Sievers, S., Waldmann, H., Giera, M., Sundström, M., Berg, L., Huber, K., “Phenomics-based Discovery of Novel Orthosteric Choline Kinase Inhibitors”. Angewandte Chemie International Edition, 2025, 64(7):e202420149. PMID:39740997
Tian, Y.; Bhattacharya, R.; Yoo, S.; Jiang, F.; Park, E.; Laragranados, G.; Shen, Y.; Park, K.-S.; Kaniskan, H. U,; Jin, J.; Hopkins, B.; Zhu, J.; Watanabe, H.*. “Epigenomic Analysis Identifies DTP Subpopulation Using HOPX to Develop Targeted Therapy Resistance in Lung Adenocarcinoma ”, iScience , 2025, 28(5):112387. PMCID: PMC12063144.
Muneer, A.; Xie, L.; Xie, X.; Zhang, F.; Wrobel, J. A.; Xiong, Y.; Yu, X.; Wang. C.; Gheorghe, C.; Wu, P.; Song, J.; Ming, G. L.; Jin, J.; Song, H.; Shi, P. Y.; Chen, X.* “Targeting G9a-m6A translational mechanism of SARS-CoV-2 pathogenesis for multifaceted therapeutics of COVID-19 and its sequalae” , iScience, 2025, 28(6):112632. PMCID: PMC12159498.
2024
Inuzuka, H; Qian, Chao; Qi,Y; Xiong, Y; Wang, C;Wang,Z; Zhang, D;Zhang, C; Jin, J*; Wei, W*; ACS Pharmacology & Translational Science , “Targeted Degradation of Receptor-Interacting Protein Kinase 1 to Modulate the Necroptosis Pathway”, 2024, 7, 3518-3526. PMCID: PMC11555510.
Corbin, J.; Yu, X.; Cai, L.; Jin, J.; Wang, G. G.* Oncogene , “EZH2 PROTACs target EZH2- and FOXM1-associated oncogenic nodes, suppressing breast cancer cell growth”, 2024, 43, 2722-2736. PMID:39112519
Nigam, A. K.; Hurley, M. F. D.; Lid, F.; Konkoľováe, E.; Klímae, M.; Trylčováe, J.; Pollice, R.; Çinaroǧluh, S. S.; Levin-Konigsbergb, R.; Handjayafg, J.; Schapiradi, M.; Chaud, R.; Perveen, S.; Ho-Leung Ng, H.; Kaniskan, Ü.; Hank, Y.; Singhl, S.; Gorgullamno, C.; Kundajeab, A.; Jin, J.; Voelz, V. A.; Webere, J.; Nenckae, R.; Bourae, E.; Vedadi, M.*; Aspuru-Guzik, A.* Digital Discovery , “Application of established computational techniques to identify potential SARS-CoV-2 Nsp14-MTase inhibitors in low data regimes”. 2024, 3, 1327-1341. doi: https://doi.org/10.1016/j.chembiol.2024.10.008
Xue Z; Qin L; Xuan H.; Luo K.; Huang M; Xie, L; Su, Y.; Xu L; Harsh, J.; Dale, B.; Shi, X.; Chen, X.; Kaniskan, HÜ.; Jin, J*., Wen, H.*, Science Advances, “A potent and selective ENL degrader suppresses oncogenic gene expression and leukemia progression”. 2024 Aug 30;10(35).eado1432. PMID:39196923. PMCID: PMC11352836
Graboski, A.L.;Simpson,J.B.; Pellock;S.J.; Mehta, N.; Creekmore, B.C.; Ariyarathna; Y.; Bhatt, A.P.; Jariwala,P.B.; Sekela, J.J.; Kowalewski, M.E.; Barker, N.K.; Mordant, A.L.; Borlandelli, V.B.; Overkleeft, H.; Herring, L.E.; Jin, J.; I James L, Redinbo,M.R. RSC Chemical Biology Journal “Advanced piperazine-containing inhibitors target microbial β-glucuronidases linked to gut toxicity.” PMID: 39211470; PubMed Central PMCID: PMC11353122. RSC Chem Biol. 2024 Jul 16;5(9):853-865
Hu,X; Kabir, M; Lin, Y; Xiong Y; Parsons, R; Gu, W; Jin, J*. Journal of Medicinal Chemistry “Design, Synthesis, and Evaluation of p53Y220C Acetylation Targeting Chimeras (AceTACs)”, , August, 2024, 67, 14633−14648 PMID:39169826.
Wang, S, E.; Xiong, Y.;Jang, M, A,; Park, K, S.; Donahue, M.; Velez J.; Jin J.*; Jiang, Y, H.*, Molecular Therapy, “Newly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome”, 2024 Aug 7;32(8):2662-2675. PMID: 38796700;.doi: https://doi.org/doi: 10.1016/j.ymthe.2024.05.034
Kabir, M.; Qin, L.; Luo, K.; Xiong, Y.; Sidi, R. A.; Park, K.-S.*; Jin, J.*, “Discovery and characterization of a novel Cereblon-recruiting PRC1 bridged PROTAC degrader.” Journal of Medicinal Chemistry. 2024, 67:6880-6892. PMID: 38607318.
Velez, J.; Han, Y.; Yim, H.; Yang, P.; Deng, Z.; Park, K.-s.; Kabir, M.; Kaniskan, H. Ü.; Xiong, Y.*; Jin, J.*, Discovery of the first-in-class G9a/GLP PROTAC degrader. Journal of Medicinal Chemistry. 2024, 67(8):6397-6409. PMID: 28602846.
Kim, Y.; Gumpper, R. H.; Liu, Y; Kocak, D. D.; Xiong, Y.; Cao, C.; Deng, Z.; Krumm, B. E.; Jain, M. K.; Zhang, S.; Jin, J.; Roth, B. L., Nature “Bitter taste receptor activation by cholesterol and an intracellular tastant.” 2024, 628(8008):664-671. PMID: 38600377.
Liu, J; Hu, X.; Luo, K; Xiong, Y; Chen, L.; Wang, Z.; Inuzuka, H.; Qian, C.; Yu, X.; Xie, L.; Muneer, A.; Zhang, D.; Paulo, J. A.; Chen, X.; Jin, J.*; Wei, W.*, Journal of the American Chemical Society“, USP7-based deubiquitinase-targeting chimeras stabilize AMPK.” 2024, 146, 16, 11507–11514; PMID: 38597345.
Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Gamble, V.; Park, K.-s.; Fagan, V.; Li, F.; Chau, I.; Vedadi, M.; Arrowsmith, C. H.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U. *; Schüle, R. *; Jin, J. *, Discovery of a potent, selective, and cell-active SPIN1 inhibitor. Journal of Medicinal Chemistry. 2024, 67(7):5837-5853. PMID: 38533580.
Nylund, P.; Garrido-Zabala, B.; Párraga, A. A.; Vasquez, L.; Pyl, P. T.; Harinck, G. M.; Ma, A.; Jin, J.; Öberg, F.; Kalushkova, A.; Wiklund, H. J.*, PVT1 interacts with polycomb repressive complex 2 to suppress genomic regions with pro-apoptotic and tumour suppressor functions in multiple myeloma. Haematologica, 2024, 109 (2): 567-577. PMID: 37496441.
Wang, Z.; Zhang, D.; Qiu, X.; Inuzuka, H.; Xiong, Y.; Liu, J.; Chen, L.; Chen, H.; Xie, L.; Kaniskan, H. Ü.; Chen, X.; Jin, J. *; Wei, W. *, Journal of the American Chemical Society . “Structurally specific Z-DNA proteolysis targeting chimera enables targeted degradation of adenosine deaminase acting on RNA”, 2024, 146 (11): 7584-7593. PMID: 38469801.
Velez, J.; Dale, B.; Park, K.-S.; Kaniskan, H. Ü.; Yu, X. *; Jin, J. *, “Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2”. European Journal of Medicinal Chemistry,. 2024, 267, 116154. PMID: 38602846.,
2023
Dang, F.; Bai, L.; Dong, J.; Hu, X.; Wang, J.; Paulo, J. A.; Xiong, Y.; Liang, X.; Sun, Y.; Chen, Y.; Guo, M.; Wang, X.; Huang, Z.; Inuzuka, H.; Chen, L.; Chu, C.; Liu, J.; Zhang, T.; Rezaeian, A.-H.; Liu, J.; Kaniskan, H. Ü.; Zhong, B.; Zhang, J.; Letko, M.; Jin, J. *; Lan, K. *; Wei, W. *, USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice. Science Translational Medicine. 2023, 15 (725): eadh7668. PMID: 38055802.
Yu, X.; Li, D.; Kottur, J.; Kim, H. S.; Herring, L. E.; Yu, Y.; Xie, L.; Hu, X.; Chen, X.; Cai, L.; Liu, J.; Aggarwal, A. K.; Wang, G. G. *; Jin, J.*, Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer. Journal of Medicinal Chemistry. 2023, 66(23): 16168–16186. PMID: 38019706.
Umaña, J.D.; Wasserman S.R.; Song L; Goel A.A; Yu X.; Jin J; Hathaway N.A. *, Chemical Epigenetic Regulation of Adeno-Associated Virus Delivered Transgenes. Human Gene Therapy. 2023, 34(17-18): 947-957. PMID: 37624737.
Pogorelov, V. M.*; Martini, M. L.; Jin, J.; Wetsel, W. C.;* Caron, M. G., Dopamine-Depleted Dopamine Transporter Knockout (DDD) Mice: Dyskinesia with L-DOPA and Dopamine D1 Agonists. Biomolecules, 2023, 13(11): 1658. PMID: 38002340.
Muneer, A.;Wang, L.; Xie, L.; Zhang, F.; Wu, B.; Mei, L.; Lenarcic, E. M.; Feng, E. H.; Song, J.; Xiong, Y.; Yu, X.; Wang, C.; Jain, K.; Strahl, B.; Cook, J. G.; Wan, Y. Y.; Moorman, N. J.; Song, H.; Jin, J.; Chen, X. *, “Non-canonical function of histone methyltransferase G9a in the translational regulation of chronic inflammation.” Cell Chemical Biology, 2023, 30:1525-1541.e7. PMID: 37858336.
Gray, Z. H.;Chakraborty, D.; Duttweiler, R. R.; Alekbaeva, G. D.; Murphy, S. E.; Chetal, K.; Ji, F.; Ferman, B. I.; Honer, M. A.; Wang, Z.; Myers, C.; Sun, R.; Kaniskan, H. Ü.; Toma, M. M.; Bondarenko, E. A.; Santoro, J. N.; Miranda, C.; Dillingham, M. E.; Tang, R.; Gozani, O.; Jin, J.; Skorski, T.; Duy, C.; Lee, H.; Sadreyev, R. I.; Whetstine, J. R.*, Epigenetic balance ensures mechanistic control of MLL amplification and rearrangement. Cell, 2023, 186(21):4528-4545.e18. PMID: 37788669.
Wang Z.; Liu J.; Qiu X.; Zhang D.; Inuzuka H.; Chen L.; Chen H.; Xie L.; Kaniskan HÜ.; Chen X.; Jin J.* ; Wei W.* , Methylated Nucleotide-Based Proteolysis-Targeting Chimera Enables Targeted Degradation of Methyl-CpG-Binding Protein 2. Journal of the American Chemical Society . 2023, 145(40): 21871–21878. PMID: 37774414.
Salas-Estrada, L.; Provasi, D.; Qiu, X.; Kaniskan, H. Ü.; Huang, X. P.; DiBerto, J. F.; Lamim Ribeiro, J. M.; Jin, J.; Roth, B. L.; Filizola, M.; De Novo Design of κ-Opioid Receptor Antagonists Using a Generative Deep-Learning Framework. Journal of Chemical Information and Modeling, 63(16): 5056–5065. PMID: 37555591.
Rialdi, A.; Duffy, M.; Scopton, A. P.; Fonseca, F.; Zhao, J. N.; Schwarz, M.; Molina-Sanchez, P.; Mzoughi, S.; Arceci, E.; Abril-Fornaguera, J.; Meadows, A.; Ruiz de Galarreta, M.; Torre, D.; Reyes, K.; Lim, Y. T.; Rosemann, F.; Khan, Z. M.; Mohammed, K.; Wang, X.; Yu, X.; Jin, J.; Guccione, E; Dar, A. C.; WNTinib is a multi-kinase inhibitor with specificity against β-catenin mutant hepatocellular carcinoma. Nature cancer, 2023, 4(8):1157-1175. PMID: 37537299.
Gao, J.; Yang, L.; Lei, S.; Zhou, F.; Nie, H.; Peng, B.; Xu, T.; Chen, X.; Yang, X.; Sheng, C.; Rao, Y.; Pu, K.; Jin, J.; Xu, Z.; Yu, H.; Stimuli-activatable PROTACs for precise protein degradation and cancer therapy. Science bulletin, 2023, 68(10): 1069–1085. PMID: 37169612.
Kabir, M.; Sun, N.; Hu, X.; Martin, T. C.; Yi, J.; Zhong, Y.; Xiong, Y.; Kaniskan, H. Ü.; Gu, W.; Parsons, R.; Jin, J.*; Acetylation Targeting Chimera Enables Acetylation of the Tumor Suppressor p53. Journal of the American Chemical Society 2023, 145(27):14932-14944. PMID: 37365684.
Velez, J.; Kaniskan, H. Ü.*; Jin, J.*; Recent advances in developing degraders & inhibitors of lysine methyltransferases. Current Opinion in Chemical Biology, 2023, 76:102356. PMID: 37379717.
Schwalm, M. P.; Krämer, A.; Dölle, A.; Weckesser, J.; Yu, X.; Jin, J.; Saxena, K.; Knapp, S.; Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization. Cell Chemical Biology, 2023, 30:753-765.e8. PMID: 37354907.
Kabir, M.; Yu, X.; Kaniskan, H. Ü.*; Jin, J.*; Chemically induced degradation of epigenetic targets. Chemical Society Reviews, 2023, 52(13):4313-4342. PMID: 37314393.
Zhao, N.; Ho, J. S. Y.; Meng, F.; Zheng, S.; Kurland, A. P.; Tian, L.; Rea-Moreno, M.; Song, X.; Seo, J. S.; Kaniskan, H. Ü.; Te Velthuis, A. J. W.; Tortorella, D.; Chen, Y. W.; Johnson, J. R.; Jin, J.*; Marazzi, I.*; Generation of host-directed and virus-specific antivirals using targeted protein degradation promoted by small molecules and viral RNA mimics. Cell Host Microbe, 2023, 31(7):1154-1169.e10. PMID: 37339625.
Yi, J.; Li, H.; Chu, B.; Kon, N.; Hu, X.; Hu, J.; Xiong, Y.; Kaniskan, H. U.; Jin, J.; Gu, W*; Inhibition of USP7 induces p53-independent tumor growth suppression in triple-negative breast cancers by destabilizing FOXM1. Cell Death & Differentiation, 2023, 30(7):1799-1810. PMID: 37291217.
Singh, I.; Li, F.; Fink, E. A.; Chau, I.; Li, A.; Rodriguez-Hernández, A.; Glenn, I.; Zapatero-Belinchón, F. J.; Rodriguez, M. L.; Devkota, K.; Deng, Z.; White, K.; Wan, X.; Tolmachova, N. A.; Moroz, Y. S.; Kaniskan, H. Ü.; Ott, M.; García-Sastre, A.; Jin, J.; Fujimori, D. G.; Shoichet, B. K.*; Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase. J. Med. Chem, 2023, 66(12):7785-7803. PMID: 37294077.
Wang, Z.; Liu, J.; Chen, H.; Qiu, X.; Xie, L.; Kaniskan, H. Ü.; Chen, X.; Jin, J.*; Wei, W.*; Telomere Targeting Chimera Enables Targeted Destruction of Telomeric Repeat-Binding Factor Proteins. Journal of the American Chemical Society. 2023, 145(19):10872-10879. PMID: 37141574.
Qiang, N.; Ao, J.; Nakamura, M.*; Chiba, T.; Kusakabe, Y.; Kaneko, T.; Kurosugi, A.; Kogure, T.; Ma, Y.; Zhang, J.; Ogawa, K.; Kan, M.; Iwanaga, T.; Sakuma, T.; Kanayama, K.; Kanzaki, H.; Kojima, R.; Nakagawa, R.; Kondo, T.; Nakamoto, S.; … Jin, J.; Kato, N.; Alteration of the tumor microenvironment by pharmacological inhibition of EZH2 in hepatocellular carcinoma. Int immunopharmacol. 2023, 118:110068. PMID: 37001386.
Vital, T.; Wali, A.; Butler, K. V.; Xiong, Y.; Foster, J. P.; Marcel, S. S.; McFadden, A. W.; Nguyen, V. U.; Bailey, B. M.; Lamb, K. N.; James, L. I.; Frye, S. V.; Mosely, A. L.; Jin, J.; Pattenden, S. G.; Davis, I. J.*; MS0621, a novel small-molecule modulator of Ewing sarcoma chromatin accessibility, interacts with an RNA-associated macromolecular complex and influences RNA splicing. Frontiers in Oncology, 2023, 13:1099550. PMID: 36793594.
Yu, X.; Wang, J.; Gong, W.; Ma, A.; Shen, Y.; Zhang, C.; Liu, X.; Cai, L.; Liu, J.; Wang, G. G.*; Jin, J.*; Dissecting and targeting noncanonical functions of EZH2 in multiple myeloma via an EZH2 degrader. Oncogene, 2023, 42(13):994-1009. PMID: 36747009.
Park, K. S.; Qin, L.; Kabir, M.; Luo, K.; Dale, B.; Zhong, Y.; Kim, A.; Wang, G. G.; Kaniskan, H. Ü.; Jin, J*; Targeted Degradation of PRC1 Components, BMI1 and RING1B, via a Novel Protein Complex Degrader Strategy. Advanced science (Weinheim, Baden-Württemberg, Germany). 2023, 10(10):e2205573. PMID: 36737841.
Sun, N.; Kabir, M.; Lee, Y.; Xie, L.; Hu, X.; Velez, J.; Chen, X.; Kaniskan, H. Ü.*; & Jin, J*; Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer. Journal of Medicinal Chemistry. 2023, 66(1):596-610. PMID: 36538511.
Marcellino, B. K.; Yang, X.; Ümit Kaniskan, H.; Brady, C.; Chen, H.; Chen, K.; Qiu, X.; Clementelli, C.; Herschbein, L.; Li, Z.; Elghaity-Beckley, S.; Arandela, J.; Kelly, B.; Hoffman, R.; Liu, J.; Xiong, Y.; Jin, J.*; Shih, A. H.*; An MDM2 degrader for treatment of acute leukemias. Leukemia, 2023, 37(2):370-378. PMID: 36309559
2022 (showing 10 out of 20 papers)
Xiong, Y.; Zhong, Y.; Yim, H.; Yang, X.; Park, K. S.; Xie, L.; Poulikakos, P. I.; Han, X.; Xiong, Y.; Chen, X.; Liu, J.; Jin, J.*; “Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets.” Journal of the American Chemical Society. 2022, 144(49):22622-22632. PMID: 36448571.
Yu, X.; Cheng, M.; Lu, K.; Shen, Y.; Zhong, Y.; Liu, J.*; Xiong, Y.*; Jin, J.*, “Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras” , Journal of Medicinal Chemistry , 2022, volume 65, 8416-8443., DOI: https://doi.org/https://doi.org/10.1021/acs.jmedchem.2c00345
Wang, J.; Park, K. S.; Yu, X.; Gong, W.; Earp, H. S.; Wang, G. G.*; Jin, J.; * Cai, L.*; A cryptic transactivation domain of EZH2 binds AR and AR’s splice variant, promoting oncogene activation and tumorous transformation. Nucleic acids research, 2022, 50(19):10929-10946. PMID: 36300627.
Yu, X.; Xu, J.; Cahuzac, K. M.; Xie, L.; Shen, Y.; Chen, X.; Liu, J.*; Parsons, R. E.*; Jin, J*; Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells. Journal of Medicinal Chemistry, 2022, 65(20):14237-14260. PMID: 36197750.
Meng, F.; Xu, C.; Park, K. S.; Kaniskan, H. U.*; Wang, G. G.* Jin, J.*; Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos. Journal of Medicinal Chemistry. 2022, 65(15), 10611-10625. PMID: 35895319.
Park, K. S.; Xiong, Y.*; Yim, H.; Velez, J.; Babault, N.; Kumar, P.; Liu, J.; Jin, J.*; Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. Journal of Medicinal Chemistry. 2022, 65, 10506-10522. PMID: 35763668.
Liu, J.; Yu, X.; Chen, H.; Kaniskan H. Ü.; Xie, L.; Chen, X.; Jin, J*.; Wei, W*.; TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors. Journal of the American Chemical Society. 2022, 144, 12934-12941. PMID: 35786952.
Dale, B.; Anderson, C.; Park, K. S.; Kaniskan H. U.; Ma, A.; Shen Y.; Zhang, C.; Xie, L.; Chen, X.; Yu, X.*; Jin, J.*; Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2. ACS Pharmacol. Transl. Sci. 2022, 5, 7, 491–507. PMID: 358337138
https://doi.org/https://doi.org/10.1021/acsptsci.2c00100
Xiong, Y.; Zhong, Y.; Yim, H.; Yang, X.; Park, K.-S.; Xie, L.; Poulikakos, P. I.; Han, X.; Xiong, Y.; Chen, X.; Liu, J.; Jin, J.* ; “Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets”. Journal of the American Chemical Society, 2022, 144: 22622–22632.. DOI: https://doi.org/https://doi.org/https://doi.org/10.1021/jacs.2c09255
2021 (showing 10 out of 29 papers)
Yu, X.; Li, D.; Kottur, J.; Shen, Y.; Kim, H. S.; Park, K. S.; Tsai, Y. H.; Gong, W.; Wang, J.; Suzuki, K.; Parker, J.; Herring, L.; Kaniskan, H. Ü.; Cai, L.; Jain, R.; Liu, J.; Aggarwal, A.; Wang, G. G.*; Jin, J.* A Selective WDR5 Degrader Inhibits Acute Myeloid Leukemia in Patient-derived Mouse Models. Science Translational Medicine, 2021, 13, eabj1578.
PMID: 34586829
Wei, J.; Meng, F.; Park, K.-S.; Yim, H.; Velez, J.; Kumar, P.; Wang, L.; Xie, L.; Chen, H.; Shen, Y.; Teichman, E.; Li, D.; Wang, G. G.; Chen, X. Kaniskan, H. U.*; Jin, J.* “Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation” Journal of the American Chemical Society , 2021, 143, 15073-15083.
PMID: 34520194 PMCID: PMC8480205.
Yu, X.; Xu, J.; Xie, L.; Wang, L.; Shen, Y.; Cahuzac, K.; Chen, X.; Liu, J.*; Parsons, R.*; Jin, J.* Design, Synthesis and Evaluation of Potent, Selective and Bioavailable AKT Kinase Degraders. J. Med. Chem. 2021, 64, 18054-18081. PMID: 34855399.
Xu, J.; Yu, X.; Martin, T. C.; Bansal, A.; Cheung, K.; Lubin, A.; Stratikopoulos, E.; Cahuzac, K. M.; Wang, L.; Xie, L.; Zhou, R.; Shen, Y.; Wu, X.; Yao, S.; Qiao, R.; Poulikakos, P. I.; Chen, X.; Liu, J., Jin, J.*; Parsons, R.* AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway Mutant Cancers with Wild Type KRAS and BRAF by Destabilizing Aurora Kinase B, Cancer Discovery , 2021, 11, 3064-3089. PMID:
34301793PMCID: PMC9056008.
Chen, H.; Liu, J.; Kaniskan, H. U.; Wei, W.*; Jin, J.* “Folate-Guided Protein Degradation by Immunomodulatory Imide Drug-Based Molecular Glues and Proteolysis Targeting Chimeras” Journal of Medicinal Chemistry, 2021, 64, 12273-12285. PMID: 34378936 PMCID: PMC8409242.
Dale, B.; Cheng, M.; Park, K.-S.; Kaniskan, H. Ü.; Xiong, Y.*; Jin, J.* “Advancing Targeted Protein Degradation for Cancer Therapy” Nature Reviews Cancer , 2021, 21, 638-654. PMID: 34131295 PMCID: PMC8463487.
Shen, Y.; Li, F.; Szewczyk, M. M.; Halabelian, L.; Chau, I.; Eram, M. S.; Dela Sena, C.; Park, K.-S.; Meng, F.; Chen, H.; Zeng, H.; McLeod, D.; Zepeda-Velazquez, C. A.; Campbell, R. M.; Mader, M. M.; Watson, B. M.; Schapira, M.; Arrowsmith, C. H.; Al-Awar, R.; Barsyte-Lovejoy, D.; Kaniskan, H. U.; Brown, P. J.*; Vedadi, M.*; Jin, J.* “A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6” Journal of Medicinal Chemistry, 2021, 64, 3697-3796. PMID: 33591753
Liu, J.; Chen, H.; Liu, Y.; Shen, Y.; Meng, F.; Kaniskan, H. U.; Jin, J.*; Wei, W.* “Cancer Selective Target Degradation by Folate-caged PROTACs”. Journal of the American Chemical Society, 2021, 143, 7380-7387. PMID: 33970635 PMCID: PMC8219215.
Bhat, K. P.; Kaniskan, H. Ü.; Jin, J.*; Gozani, O.* “Epigenetics and Beyond: Targeting Writers of Protein Lysine Methylation to Treat Disease” Nature Reviews Drug Discovery, 2021, 20, 265-286. PMCID: PMC8035146.
Liu, J.; Chen, H.; Kaniskan, H. U.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.* “TF-PROTACs Enable Targeted Degradation of Transcription Factors” Journal of the American Chemical Society, 2021, 143, 8902-8910.
PMID: 34100597 PMCID: PMC8225582
For papers published before 2021, please see Dr. Jin’s full publication list